BIOLOGICALLY ACTIVE CYCLIZED POLYPEPTIDE - YISSUM RES DEV CO OF HEBREW UNIV OF JERUSALEM

Title:

BIOLOGICALLY ACTIVE CYCLIZED POLYPEPTIDE

Document Type and Number:

Japanese Patent JP3509029

Kind Code:

B2

Abstract:

PURPOSE: To obtain a new biologically active cyclized polypeptide having a cyclized backbone used as a metabolically stable NK-1 acceptor selectivity tachykinin agonist for the treatment of ache, inflamation, Parkinson's disease, Alzheimer disease, etc.
CONSTITUTION: A compd. of formula I [where (q) is 2-10; each of G and L is a protecting group; and R is a naturally occurring or synthetic amino acid side-chain] is reacted with an amino acid or a polypeptide of formula II [where A'A' is a naturally occurring or synthetic amino acid residue; (m) is 0 or 1-10; and E is a carboxyl protecting group] to form a compd. of formula III (where A1A1 is the same as A'A') and the protecting group L is selectively released. The resultant compd. is reacted with an amino acid or a peptide of formula IV [where AA is a naturally occurring or synthetic amino acid residue; (n) is 1-10; and J is a protecting group] and the protecting group J is released. The resultant compd. is reacted with an aliphatic dicarboxylic acid, the protecting group G is released to form a compd. of formula V and this compd. is subjected to intramolecular condensation in the presence of dicyclohexylcarbodiimide to obtain the objective compd. of formula VI [where the semicircle designates a group of formula VII (where M is CONH or the like); and (p) is 2-10].

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Inventors:

Gilon, Chaim
Zelinger, Zvi
Byk, Gerardo

Application Number:

JP30434792A

Publication Date:

March 22, 2004

Filing Date:

October 02, 1992

Export Citation:

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Assignee:

YISSUM RES DEV CO OF HEBREW UNIV OF JERUSALEM

International Classes:

A61P25/28; A61P29/00; C07K1/06; C07K1/10; A61K38/00; C07K1/113; C07K7/22; C07K7/52; C07K7/56; (IPC1-7): C07K7/52; C07K1/06; C07K1/10

Other References:

Ｂｉｏｐｏｌｙｍｅｒｓ，Ｖｏｌ．３１，Ｎｏ．６（１９９１．Ｍａｙ）ｐ．７４５−７５０
Ｐｅｐｔ．：Ｃｈｅｍ．，Ｓｔｒｕｃｔ．Ｂｉｏｌ．，Ｐｒｏｃ．Ａｍ．Ｐｅｐｔ．Ｓｙｍｐ．，１１ｔｈ，ｐ．９８４−９８５

Attorney, Agent or Firm:

浅村皓（外３名）

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